Absorption Sitagliptin is rapidly absorbed, with 100 mg reaching a C max of 950 nM in 1 to 4 h. The bioavailability is approximately 87%.
Distribution Vd is approximately 198 L. Plasma protein binding is 38%.
Metabolism Metabolism by CYP3A4 and, to a lesser degree, CYP2C8 is a minor pathway in the Cl of sitagliptin.
Elimination Terminal t ½ is approximately 12.4 h. Approximately 13% is excreted in feces and 87% in urine via active tubular secretion (79% as unchanged drug). Sitagliptin is a substrate for organic anion transport.
|